9ewa: Difference between revisions
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The | ==The sTeLIC pentameric Ligand-Gated Ion Channel (wild-type) in complex with 4-Bromophenethylamine== | ||
<StructureSection load='9ewa' size='340' side='right'caption='[[9ewa]], [[Resolution|resolution]] 3.01Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[9ewa]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Endosymbiont_of_Tevnia_jerichonana_(vent_Tica) Endosymbiont of Tevnia jerichonana (vent Tica)]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=9EWA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9EWA FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.006Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BNG:B-NONYLGLUCOSIDE'>BNG</scene>, <scene name='pdbligand=VMT:2-(4-bromophenyl)ethanamine'>VMT</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=9ewa FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9ewa OCA], [https://pdbe.org/9ewa PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9ewa RCSB], [https://www.ebi.ac.uk/pdbsum/9ewa PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9ewa ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/G2FID1_9GAMM G2FID1_9GAMM] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
BACKGROUND AND PURPOSE: Allosteric modulation of pentameric ligand-gated ion channels (pLGICs) are critical for the action of neurotransmitters and many psychoactive drugs. However, details of their modulatory mechanisms remain unclear, especially beyond the orthosteric neurotransmitter-binding sites. The recently reported prokaryotic symbiont of Tevnia jerichonana ligand-gated ion channel (sTeLIC), a pH-gated homologue of eukaryotic receptors in the pLGIC family, is thought to be modulated by aromatic compounds via a relatively uncharacterised modulatory site in the extracellular vestibule. EXPERIMENTAL APPROACH: We have characterised the effects of psychostimulant derivatives on sTeLIC using two-electrode voltage-clamp electrophysiology in the presence and absence of engineered mutations, and determined X-ray and cryo-EM structures of the channel in both closed and open states. KEY RESULTS: We have shown that sTeLIC is sensitive to potentiation by several amphiphilic compounds, which preferentially bind to a vestibular pocket in the contracted open-state extracellular domain. CONCLUSIONS AND IMPLICATIONS: This work provides a detailed structure-function mechanism for allosteric potentiation via a noncanonical ligand site, with potential conservation of the eukaryotic pentameric ligand-gated ion channels. | |||
Vestibular modulation by stimulant derivatives in a pentameric ligand-gated ion channel.,Karlsson E, Anden O, Fan C, Fourati Z, Haouz A, Zhuang Y, Howard RJ, Delarue M, Lindahl E Br J Pharmacol. 2025 Mar 11. doi: 10.1111/bph.70011. PMID:40065647<ref>PMID:40065647</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 9ewa" style="background-color:#fffaf0;"></div> | ||
[[Category: | == References == | ||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Large Structures]] | |||
[[Category: Delarue M]] | |||
[[Category: Fourati Z]] | |||
